B3-adrenoceptor agonists and antagonists for the treatment...

A - Human Necessities – 61 – K

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A61K 31/34 (2006.01) A61K 31/343 (2006.01) A61K 31/40 (2006.01) A61K 31/4025 (2006.01) A61K 31/404 (2006.01) A61K 31/42 (2006.01) A61K 31/422 (2006.01) A61K 31/4245 (2006.01) A61K 31/425 (2006.01) A61K 31/427 (2006.01)

Patent

CA 2158910

Disclosed are pharmaceutical compositions for treat- ing or preventing intestinal motility disorders such as irritable bowel syndrome, peptic ulceration, esophagitis, gastritis and duodenitis, (including that induced by H. pylori), intestinal ulcerations (including inflammatory bowel disease, ulcerative colitis, Crohn's disease and proctitis), gastrointestinal ulcerations, depression, prostate disease, neurogenetic inflammation and dyslipidemia comprising a .beta.3- adrenoceptor antagonist or agonist, which may for example be a compound of the formula: Image Image (wherein R1 is phenyl, (CH2)n-O-phenyl or thiazolyl, each optionally substituted, R2 is hydrogen or alkyl, R3 is hydrogen or substituent, R4 is, for example, (CH2)n-CN, R5 is hydrogen or alkyl, X is bond, O or S, Z is C or N, and Y is O, N or S).

On divulgue des compositions pharmaceutiques pour traiter ou prévenir les troubles de la motilité intestinale comme le côlon irritable, l'ulcère gastro-duodénal, l'oesophagite, la gastrite et la duodénite, (y compris les troubles provoqués par H. pylori), les ulcères intestinaux (y compris la maladie intestinale inflammatoire, la colite ulcérative, la maladie de Crohn et la rectite), les ulcères gastro-intestinaux, la dépression, la prostatopathie, l'inflammation neurogène et la dyslipidémie, lesquelles compositions comprennent un antagoniste ou un agoniste du récepteur adrénergique bêta 3 qui peut, par exemple, être un composé de formule : Image Image (où R1 est un phényle, (CH2)n-O-phényle ou thiazolyle, pouvant tous être substitués, R2 est un atome d'hydrogène ou un groupe alkyle, R3 est un hydrogène ou un substituant, R4 est, par exemple, (CH2)n-CN, R5 est un hydrogène ou un alkyle, X est une liaison, O ou S, Z est C ou N, et Y est O, N ou S).

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